| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
RAF[1]
RAF (BRAF-V600E) |
|---|---|
| ln Vitro |
In BRAFV600E cell lines, PLX7922 (1–1000 nM) suppresses pERK, whereas in mutant NRAS cell lines (B9 and IPC-298), pERK is activated[1].
In BRAF‑V600E cell lines (e.g., A375), PLX7922 (1‑1000 nM) suppresses pERK in a concentration‑dependent manner. In contrast, in mutant NRAS cell lines (e.g., B9 and IPC‑298), PLX7922 activates pERK. This paradoxical activation is characteristic of certain RAF inhibitors that induce RAF dimerization. |
| ln Vivo |
No detailed in vivo activity data for PLX7922 has been reported. As a tool compound, it has been used in animal models of melanoma to study the in vivo effects of RAF inhibition on pERK levels and tumor growth. The paradoxical activation observed in NRAS‑mutant cells may limit its therapeutic utility in certain genetic contexts.
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| Enzyme Assay |
For non‑cellular assays, recombinant BRAF‑V600E protein is incubated with PLX7922 (0.1‑1000 nM) in the presence of ATP and a substrate (e.g., MEK). Kinase activity is measured by quantifying phosphorylated MEK via Western blotting, ELISA, or radiometric methods. Binding affinity can be determined by SPR or fluorescence polarization.
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| Cell Assay |
PLX7922 is dissolved in DMSO and diluted in cell culture media (final DMSO ≤0.1%). BRAF‑V600E mutant melanoma cells (e.g., A375) or NRAS‑mutant cell lines (e.g., B9, IPC-298) are treated with PLX7922 (1‑1000 nM) for 2‑24 h. pERK levels are measured by Western blotting. Cell proliferation is assessed by MTT or colony formation assays.
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| Animal Protocol |
No detailed in vivo protocol for PLX7922 has been reported. For standard RAF inhibitors, the compound would be formulated in a suitable vehicle (e.g., 0.5% methylcellulose or 10% DMSO/40% PEG400/5% Tween 80) and administered orally or intraperitoneally to mice bearing BRAF‑V600E melanoma xenografts. pERK levels in tumors and pharmacokinetics would be assessed.
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| ADME/Pharmacokinetics |
No PK data for PLX7922 has been reported. As a small‑molecule RAF inhibitor, it is expected to have moderate oral bioavailability. Detailed parameters such as half‑life, Cmax, and clearance are not publicly available. Solubility: DMSO up to 100 mg/mL (215.25 mM).
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| Toxicity/Toxicokinetics |
No toxicity data for PLX7922 has been reported. As a RAF inhibitor, potential toxicities may include skin rash, hyperkeratosis, and paradoxical activation of the MAPK pathway in wild‑type BRAF cells or NRAS‑mutant cells. No toxicology studies have been published.
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| References | |
| Additional Infomation |
PLX7922 (CAS: 1638772-61-8; formula: C20H2₅FN₆O2S2; MW: 464.58) is a research‑use RAF inhibitor that binds to BRAF‑V600E. It is a valuable tool for studying context‑dependent effects of RAF inhibition and paradoxical MAPK activation. PLX7922 has not been approved for clinical use, and no clinical trial data has been reported.
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| Molecular Formula |
C20H25FN6O2S2
|
|---|---|
| Molecular Weight |
464.579904317856
|
| Exact Mass |
464.146
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| CAS # |
1638772-61-8
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| PubChem CID |
91971376
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| Appearance |
Off-white to light yellow solid powder
|
| LogP |
3.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
31
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| Complexity |
701
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
S1C(C2C=CN=C(N)N=2)=C(C2C=CC=C(C=2F)NS(N(C)CC)(=O)=O)N=C1C(C)(C)C
|
| InChi Key |
YBUJMZKTOUBMGW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H25FN6O2S2/c1-6-27(5)31(28,29)26-13-9-7-8-12(15(13)21)16-17(14-10-11-23-19(22)24-14)30-18(25-16)20(2,3)4/h7-11,26H,6H2,1-5H3,(H2,22,23,24)
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| Chemical Name |
5-(2-aminopyrimidin-4-yl)-2-tert-butyl-4-[3-[[ethyl(methyl)sulfamoyl]amino]-2-fluorophenyl]-1,3-thiazole
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (215.25 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1525 mL | 10.7624 mL | 21.5248 mL | |
| 5 mM | 0.4305 mL | 2.1525 mL | 4.3050 mL | |
| 10 mM | 0.2152 mL | 1.0762 mL | 2.1525 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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